NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

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A lipophilic copper(II)bis(thiosemicarbazone) labeled with the positron-emitting isotope (61)Cu with hypoxia-selective and radioisotopic activities. With a high membrane permeability and redox potential, (61)Cu-ATSM easily enters and selectively resides in hypoxic cells. The extent of (61)Cu-ATSM retention in tissue is inversely related to the state of tissue oxygenation allowing the quantitation of tissue hypoxia with positron emission tomography (PET). Check for active clinical trials using this agent. (NCI Thesaurus)

A deoxycytidine analog and high-affinity substrate for deoxycytidine kinase (DCK), labeled with fluorine F 18, with potential diagnostic activity upon positron emission tomography (PET) imaging. [18F]L-FAC is preferentially taken up by and accumulated in cells with high deoxycytidine kinase (DCK) levels, such as in tumor cells with dysregulated nucleoside metabolism. Upon uptake through the nucleoside transporter, [18F]L-FAC is phosphorylated by DCK and, subsequently, the 18F moiety can be visualized upon PET imaging. As many nucleoside analog prodrugs are chemotherapeutic agents that require DCK for activation, [18F]L-FAC can potentially be used as a marker to predict chemotherapeutic efficacy of these prodrugs. In addition, as DCK is upregulated in certain immune cells, such as activated T-cells, [18F]L-FAC can also be used to measure immune activation in response to immunomodulating agents. DCK, a rate-limiting enzyme in the nucleoside salvage pathway for DNA synthesis, is overexpressed in certain solid tumors, lymphoid and myeloid malignancies and certain immune cells, such as proliferating T-lymphocytes. Check for active clinical trials using this agent. (NCI Thesaurus)

A radioconjugate composed of 2′-deoxy-2′-18F-fluoro-5-methyl-beta-L-arabinofuranosylcytosine ([18F]L-FMAC), a L-deoxycytidine analog and high-affinity substrate for deoxycytidine kinase (DCK), labeled with fluorine F 18, with potential diagnostic activity during positron emission tomography (PET) imaging. Upon administration, [18F]L-FMAC is preferentially taken up by and accumulated in cells with high DCK levels, including tumor cells with dysregulated nucleoside metabolism. After phosphorylation by DCK, the 18F moiety can be visualized by PET imaging. As many nucleoside analog prodrugs are chemotherapeutic agents that require DCK for their phosphorylation and activation, [18F]L-FMAC can potentially be used as a marker to measure DCK activity and to predict the chemotherapeutic efficacy of DCK-dependent prodrugs. DCK, a rate-limiting enzyme in the deoxyribonucleoside salvage pathway for DNA synthesis, is overexpressed in certain solid tumors, lymphoid and myeloid malignancies and certain immune cells, such as proliferating T-lymphocytes. The L-enantiomer is less susceptible to deamination by cytidine deaminase (CDA) than the D-enantiomer and increases the stability of this radioconjugate. Check for active clinical trials using this agent. (NCI Thesaurus)

A small molecular-weight, malonic acid-based probe [(2-(5-fluoro-pentyl)-2-methyl-malonic acid or ML-10] labeled with the radioactive isotope fluorine F 18 with potential apoptosis radioimaging use. Upon administration, [F18]-ML-10 binds selectively to apoptotic cells due to apoptotic cell membrane features that differ from those of normal, healthy and necrotic cell membranes. Upon entering the apoptotic cell, this agent accumulates within the cytoplasm where it can be imaged using positron emission tomography (PET). Detection of apoptotic cells using this imaging technology may be useful in monitoring tumor responses to cytotoxic therapies. ML-10 appears to mimic the alkyl-malonic acid motif present in gamma -carboxyglutamic (Gla), an amino acid that plays a crucial role in the binding of clotting factors to negatively-charged phospholipids exposed on the surfaces of apoptotic cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A radiopharmaceutical consisting of a sulfonamide covalently attached to the positron-emitting isotope fluorine F 18 with CA-IX-binding and radioisotopic activities. Upon administration, the sulfonamide moiety of [F18]VM4-037 binds to the cell-surface tumor-associated antigen (TAA) carbonic anhydrase IX isoenzyme (CA-IX); CA-IX-expressing tumor cells can then be visualized using positron emission tomography (PET). CA-IX has been found to be elevated in a variety of hypoxic tumors; elevated CA-IX has been positively correlated with tumor growth, tumor invasion and poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)

A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata radiolabeled with carbon 11 (11C) with antineoplastic and radiotracer properties. During the S phase of the cell cycle, topotecan inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Quantitation of 11C topotecan accumulated in tumor tissues by positron emission tomography (PET) may help predict responses to topotecan therapy. Check for active clinical trials using this agent. (NCI Thesaurus)

The orally bioavailable C-4 methyl carbonate analogue of paclitaxel, labeled with radioactive carbon 14, with radioisotope and potential antineoplastic activities. 14C BMS-275183 binds to tubulin and inhibits microtubule disassembly, which may result in cell cycle arrest at the G2/M phase and inhibition of cell division, and subsequently cell death. This agent may be useful for treating multi-drug resistant (MDR) tumors because it does not appear to be a substrate for P-glycoprotein. Check for active clinical trials using this agent. (NCI Thesaurus)

A stable derivative of prostaglandin E2 (PGE2) with potential hematopoietic activity. Administration of 16,16 dimethyl-prostaglandin E2 (dmPGE2) appears to lead to increased formation of hematopoietic stem and progenitor cells. Even though the exact mechanism of action has yet to be fully elucidated, this agent may stimulate hematopoiesis by activating the Wnt signaling pathway, which increases cellular levels of beta-catenin, a subunit of the cadherin protein complex. Check for active clinical trials using this agent. (NCI Thesaurus)

A radioconjugate and an acetate analog labeled with fluorine F 18 ((18)F-FAC), a positron-emitting isotope, with potential prostate tumor tracer property using positron emission tomography (PET). Although the mechanism of action is unclear, fluorine F 18 acetate preferentially accumulates in tumor tissue, serving as a tracer for imaging tumors with PET. Fluorine 18 has a longer radioactive half-life (110 min) vs. the half-life of carbon-11 acetate (20.4 min). Furthermore, (18)F-FAC showed a rapid clearance from liver and extensive excretion to bile and urine in comparison with carbon-11 acetate, therefore this tracer may be a useful alternative to C-11 acetate for the detection of prostate tumors by PET. Check for active clinical trials using this agent. (NCI Thesaurus)

A radiofluorinated 2-nitroimidazole derivative with hypoxia-specific tracer activity. 18F-fluoroazomycin arabinoside is reduced under hypoxic conditions and is often seen in various malignant tumors, forming highly reactive intermediates. In its reduced form, 18F-fluoroazomycin arabinoside covalently binds to macromolecules, thereby accumulating in hypoxic cells and allowing radioisotopic imaging of these particular cells. Compared to 18F-misonidazole, 18F-fluoroazomycin arabinoside has a lower octanol:water partition coefficient; it therefore has less tendency to accumulate in lipophilic tissues and exhibits a faster renal clearance, leading to an improved imaging ability of hypoxic tissue. Check for active clinical trials using this agent. (NCI Thesaurus)

A radiofluorinated 2-nitroimidazole derivate with hypoxia-specific tracer activity. Misonidazole is reduced under hypoxic conditions and in reduced form covalently binds to macromolecules in hypoxic cells. 18F (fluorine-18) radiofluorination of misonidazole to form 18F-fluoromisonidazole allows radioisotopic imaging of reduced misonidazole bound to macromolecules in hypoxic cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A heparin derivative in which the 2-O and 3-O sulfate groups of heparin are removed and that lacks anticoagulant activity, with potential anti-inflammatory, immodulatory and antineoplastic activities. Upon administration, 2-O, 3-O desulfated heparin (ODSH) binds to both chemokine stromal cell-derived factor 1 (SDF-1 or CXCL12) and CXC chemokine receptor 4 (CXCR4). This prevents the interaction of CXCL12 with CXCR4, blocks CXCR4 activation, and may result in decreased proliferation and migration in CXCR4-overexpressing tumor cells. In addition, inhibition of CXCL12/CXCR4 interaction may induce mobilization of hematopoietic cells from the bone marrow into the blood. In addition, ODSH prevents the interaction of the receptor for advanced glycation end-products (RAGE) with its ligands, including advanced glycation end-products (AGEs), Mac-1(CD11b/CD18), the nuclear pro-inflammatory protein high mobility group box protein-1 (HMGB-1), carboxymethyl lysine-bovine serum albumin (CML-BSA) and members of the S100 calgranulin family. In addition, this agent inhibits the enzymes heparanase, cathepsin G, and human leukocyte elastase, which are involved in inflammation and metastasis. ODSH also binds to platelet factor 4 (PF4 or CXCL4) and may prevent PF4's inhibitory effect on platelet production. Altogether, this may inhibit tumor cell invasiveness and metastasis. ODSH also binds to platelet factor 4 (PF4 or CXCL4) and may prevent PF4's inhibitory effect on platelet production. This may increase platelet production. Unlike heparin, this agent does not induce heparin-induced thrombocytopenia (HIT). RAGE, a receptor belonging to the immunoglobulin superfamily, plays a key role in inflammation and is overexpressed in a variety of cancers. CXCR4 is a chemokine receptor belonging to the G protein-coupled receptor (GPCR) family that plays an important role in chemotaxis, chemoresistance and angiogenesis, and is upregulated in several tumor cell types. The interaction between CXCL12/CXCR4 induces retention of hematopoietic cells in the bone marrow.
Check for active clinical trials using this agent. (NCI Thesaurus)

A deoxyuridine prodrug with potential antineoplastic activity. Upon cellular uptake, 2’-F-ara-deoxyuridine (FAU) is phosphorylated by thymidine kinase to FAU monophosphate and subsequently methylated in the 5'-position by thymidylate synthase (TS) to its activated form, 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FMAUMP is incorporated into DNA leading to an inhibition of DNA synthesis and so cell growth. The catalytic activity of TS is critical to activation of FAU and subsequent incorporation into DNA. FAU may be beneficial in the case of tumors with high TS activity that are resistant to TS inhibitors. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally bioavailable fluorinated analog of fucose that is a protein fucosylation inhibitor, with potential antineoplastic and immunomodulating activities. Upon administration of SGN-2FF, 2-fluorofucose (2-FF) mimics fucose and is converted to guanosine diphosphate (GDP)-2FF, which prevents the formation of the fucosylation substrate GDP-fucose, and the incorporation of fucose into glycoproteins by fucosyltransferase. As fucosylation of glycoproteins plays a key role in many biological processes, such as protein function, receptor binding, cell signaling and cellular adhesion, and is essential for tumor progression, blocking fucosylation decreases tumor cell growth. In addition, blocking fucosylation of monoclonal antibodies generates fucose-deficient antibodies that exert enhanced antibody-dependent cell-mediated cytotoxicity (ADCC). Check for active clinical trials using this agent. (NCI Thesaurus)

A preparation of autologous human T-lymphocytes isolated from renal cell cancer (RCC) patient and transduced with 2G-1 TCR, a retroviral vector encoding the alpha and beta chains of a T-cell receptor that recognizes TNF-related apoptosis inducing ligand (TRAIL) bound to death receptor 4 (DR4), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and introduction into the RCC patient, 2G-1 TCR retroviral vector-transduced lymphocytes may stimulate a cytotoxic T lymphocyte (CTL) response against RCC cells with TRAIL bound to DR4 on their surfaces. TRAIL, a member of the TNF superfamily, is a homotrimeric type II membrane protein that rapidly induces oligomerization of receptor intracellular death domains and apoptosis in a variety of tumor cells when bound to its receptors; DR4 (TRAIL receptor 1), a member of the TNF receptor family, is overexpressed by a variety of malignant cell types. Check for active clinical trials using this agent. (NCI Thesaurus)

A ring-substituted amphetamine derivative, structurally related to the hallucinogen mescaline, with entactogenic, neurotoxic, and motor-stimulatory activities. 3,4-methylenedioxymethamphetamine (MDMA) produces an acute, rapid enhancement in both the release of serotonin from and the inhibition of serotonin reuptake by serotonergic nerve endings in the brain. Once within the cell, MDMA depletes stores of tryptophan hydroxylase (TPH) via acute oxidative inactivation; in turn, depleted stores of TPH leave cell terminals open to damage from oxidative stress, possibly a source of MDMA neurotoxicity. This agent also induces norepinephrine, dopamine, and acetylcholine release and can act directly on a number of receptors, including alpha 2-adrenergic and 5-hydroxytryptamine (5-HT) 2A receptors. MDMA may suppress the dyskinesia associated with long-term use of L-dopamine (L-DOPA) without affecting the efficacy of L-DOPA treatment. Check for active clinical trials using this agent. (NCI Thesaurus)

A hapten-carrier immunoconjugate composed of the hapten trans-3′-aminomethyl nicotine conjugated to a recombinant P. aeruginosa exoprotein A, rendered nontoxic through amino acid depletion, with potential immunostimulating activity. Upon vaccination with 3'-aminomethyl nicotine-P. aeruginosa r-exoprotein A conjugate vaccine, the immune system may produce anti-nicotine antibodies. Antibody-bound nicotine cannot pass the blood brain barrier (BBB) to activate brain nicotine receptors. Nicotine, a small organic molecule that is not
immunogenic, must be haptenized and conjugated to a carrier
protein, such as nontoxic recombinant P. aeruginosa exoprotein A, to induce an antibody response. Aluminium
hydroxide may be used as an adjuvant for this vaccine. Check for active clinical trials using this agent. (NCI Thesaurus)

A population of proprietary, off-the-shelf, three-dimensional (3D)-expanded, allogeneic placenta-derived stromal cells that can potentially be used to increase hematopoietic recovery from hematological disorders or after a hematopoietic stem cell transplant (HSCT). Upon intramuscular (IM) injection of placental expanded (PLX)-R18, these cells secrete a range of specific hematopoietic, regenerative proteins depending on their in vivo environment. The secreted proteins are involved in maintenance, renewal, proliferation, differentiation, and mobilization of hematopoietic progenitor cells (HPCs), and include, but are not limited to, granulocyte colony-stimulating factor (GCSF), monocyte chemoattractant protein-1 (MCP-1/CCL2), MCP-3 (CCL7), interleukin-6 (IL-6), and IL-8. This increases the number of colony-forming hematopoietic progenitors in the bone marrow, regenerates the bone marrow hematopoietic cells, and elevates and restores blood cell production. Check for active clinical trials using this agent. (NCI Thesaurus)

A preparation of genetically modified autologous T-lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) targeting the human tumor-associated antigen (TAA) MUC16ecto and encoding the human pro-inflammatory cytokine interleukin-12 (IL-12), fused to the signaling domain of the zeta chain of the TCR/CD3 complex (28z), and a truncated form of the human epidermal growth factor receptor (EGFRt), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, 4H11-28z/fIL-12/EGFRt-expressing autologous T-lymphocytes are directed to and induce selective toxicity in MUC16-expressing tumor cells. In addition, the T-cells secrete IL-12 which induces secretion of interferon-gamma, promotes the activation of natural killer cells (NKs), and induces cytotoxic T-cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. Devoid of both ligand binding domains and tyrosine kinase activity, the expressed EGFRt both facilitates in vivo detection of the administered, transduced T-cells and can promote elimination of those cells through a cetuximab-induced antibody-dependent cellular cytotoxicity (ADCC) response. MUC16, a transmembrane protein and glycosylated mucin, is overexpressed on the cell surface of the majority of ovarian cancer cells but not on healthy cells. MUC16ecto is the extracellular portion of MUC-16 and is the part that is retained by cells after cleavage of CA-125. Check for active clinical trials using this agent. (NCI Thesaurus)

An iodinated doxorubicin analogue with antiamyloid activity. 4'-Iodo-4'-deoxydoxorubicin (IDOX) binds with high affinity to five types of natural amyloid fibrils including immunoglobulin light chains, amyloid A, transthyretin (methionine-30 variant), ß-protein (Alzheimer), and ß2-microglobulin. This agent may inhibit fibril growth, increasing the solubility of amyloid tissue deposits and facilitating their clearance. IDOX has also been shown to insulin amyloid fibrillogenesis in vitro. Check for active clinical trials using this agent. (NCI Thesaurus)

An emulsion of 4 melanoma peptides with potential immunomodulating and antineoplastic activities. Upon vaccination, 4-peptide melanoma vaccine may stimulate an immune response against 4 different melanoma associated antigens. This may lead to a reduction in tumor cell proliferation of cancer cells expressing these antigens. Check for active clinical trials using this agent. (NCI Thesaurus)

Genetically modified autologous T lymphocytes transduced with a lentiviral vector encoding a fourth generation specific chimeric antigen receptor (4SCAR) specific for the disialoganglioside GD2 and which includes the CD3zeta chain and the signaling domains of the co-stimulatory molecules CD28, CD137, and CD27 fused with the suicide gene inducible caspase 9 (iCasp9), with potential immunomodulating and antineoplastic activities. Upon intravenous administration of 4SCAR-GD2 T cells, these cells target the GD2 antigen on tumor cells to induce selective toxicity against GD2-expressing tumor cells. The tumor-associated antigen (TAA) GD2 is overexpressed on the surface of neuroblastoma cells and by other neuroectoderm-derived neoplasms, while it is minimally expressed on normal cells. iCasp9 consists of a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V) linked to human caspase 9. If the administered T cells lead to unacceptable side effects, the chemical homodimerizer AP1903 can be administered; this binds to the drug binding FKBP12-F36V domain and activates caspase 9, which results in the apoptosis of the administered T cells and enhances safety of this agent. CD28, CD137 and CD27, T-cell surface-associated co-stimulatory molecules, are required for full T cell activation. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally bioavailable 4-thio modified 2-deoxycytidine analog, with potential antineoplastic activity. Upon administration of 4-thio-2-deoxycytidine (TdCyd), this cytidine analog is incorporated into DNA during replication and inhibits the activity of DNA methyltransferase 1 (DNMT1), which blocks DNA hypermethylation. This results in DNMT1 depletion, hypomethylation of DNA, and the reactivation of tumor suppressor genes that were silenced by hypermethylation; this results in antitumor activity and an inhibition of tumor cell proliferation.
Check for active clinical trials using this agent. (NCI Thesaurus)

The fluorine-18 (18F)-radiolabeled pyrimidine analog 5-fluorouracil (5-FU) with positron-emitting activity. Upon administration, 5-[18F]fluorouracil distribution in tumor tissue may be measured with positron emission tomography (PET). The degree of 5-[18F]fluorouracil uptake in tumor tissue may help to predict the response to 5-fluorouracil-based chemotherapy or to determine the response to other therapeutic agents used to treat 5-FU-sensitive tumors. Check for active clinical trials using this agent. (NCI Thesaurus)

An equimolar gas mixture of oxygen (O2) and nitrous oxide (N2O) with potential analgesic activity. Upon inhalation, 50% oxygen/50% nitrous oxide premix produces rapidly reversible analgesia. The exact mechanism through which nitrous oxide exerts its analgesic effect has yet to be fully elucidated, but it appears to be associated with the neuronal release of endogenous opioid peptides. Check for active clinical trials using this agent. (NCI Thesaurus)

A radioconjugate consisting of a 7 amino acid peptide sequence, KCCFPAQ, that specifically targets human colon cancer and that is labeled, via the linker, GGGSK, with the fluorescent dye, fluorescein isothiocyanate (5-FITC), with potential imaging activity. Following spray application to the colon wall during colonoscopy in areas that look abnormal, the colon heptapeptide moiety of 5-FITC-labeled colon-heptapeptide specifically targets and binds to a cell surface target overexpressed on pre-cancerous or cancerous colon cells. Upon internalization, the FITC moiety allows for fluorescent imaging and the area of interest for biopsies can then be visualized. Check for active clinical trials using this agent. (NCI Thesaurus)

A radioconjugate consisting of the 7 amino acid peptide sequence ASYNYDA (GI heptapeptide) and labeled with the fluorescent dye fluorescein isothiocyanate (5-FITC), with potential imaging activity. Upon topical application to the esophageal mucosa using a spray, the heptapeptide moiety of 5-FITC-labeled GI-heptapeptide binds to abnormal cells in the esophagus; the FITC moiety allows for imaging with white light and the area of interest for biopsies can then be visualized. Check for active clinical trials using this agent. (NCI Thesaurus)

A fluorinated pyrimidine analogue antimetabolite with potential antineoplastic activity. As a prodrug, 5-fluoro-2-deoxycytidine is converted by intracellular deaminases to the cytotoxic agent 5-fluorouracil (5-FU). 5-FU is subsequently metabolized to active metabolites including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits thymidylate synthase, thereby reducing the production of thymidine monophosphate, which leads to depletion of thymidine triphosphate and the inhibition of DNA synthesis and cell division. FUTP competes with uridine triphosphate (UTP) for incorporation into the RNA strand, which results in the inhibition of RNA and protein synthesis and cell proliferation. Other fluorouracil metabolites also get incorporated into both DNA and RNA, with further inhibition of cellular growth. Check for active clinical trials using this agent. (NCI Thesaurus)

A topical formulation containing 0.5 % of antimetabolite 5-fluorouracil (5-FU) and 10% of salicylic acid, with potential antimitotic and keratolytic activity. Upon cutaneous application, 5-FU in the 5-fluorouracil/salicylic acid topical solution impedes pyrimidine metabolism thereby inhibiting cell growth, while the salicylic acid induces anti-inflammatory response and results in keratolytic effect. This may result in the breakdown of keratinocytes and prevent proliferation of keratinocytes locally. Check for active clinical trials using this agent. (NCI Thesaurus)

A racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities. Although the exact mechanism of action is unknown, 6,8-bis(benzylthio)octanoic acid has been shown to inhibit metabolic and regulatory processes required for cell growth in solid tumors. Both enantiomers in the racemic mixture exhibit antineoplastic activity. Check for active clinical trials using this agent. (NCI Thesaurus)

A synthetic triazine analogue of uridine with antimetabolite activity. 6-azauridine inhibits de novo pyrimidine synthesis and DNA synthesis and is converted intracellularly into mono, di-, and triphosphate derivatives, which incorporate into RNA and inhibit protein synthesis. Check for active clinical trials using this agent. (NCI Thesaurus)

An inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) and derivative of 3-(3-pyridinyl)-1-[4-pyridinyl]-2-propen-1-one (3PO), with potential antineoplastic activity. Upon administration, PFKFB3 inhibitor PFK-158 binds to and inhibits the activity of PFKFB3, which leads to the inhibition of both the glycolytic pathway in and glucose uptake by cancer cells. This prevents the production of macromolecules and energy that causes the enhanced cellular proliferation in cancer cells as compared to that of normal, healthy cells. Depriving cancer cells of nutrients and energy leads to the inhibition of cancer cell growth. PFKFB3, an enzyme that catalyzes the conversion of fructose-6-phosphate to fructose-2,6-bisphosphate, is highly expressed and active in human cancer cells; it plays a key role in increasing both glycolytic flux in and proliferation of cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17bHSD5, aldo-keto reductase 1C3; AKR1C3), with potential antineoplastic activity. Upon administration, ASP9521 selectively binds to and inhibits the activity of 17bHSD5. This prevents the conversion of the adrenal androgens dehydroepiandrosterone and androstenedione into 5-androstenediol and testosterone. By blocking testosterone production, ASP9521 may inhibit the growth of testosterone-dependent cancers such as castration-resistant prostate cancer (CRPC). 17bHSD5, expressed both in normal prostate tissue and in prostate cancer (PC), plays a crucial role in persistent production of androgens despite castration; its expression is associated with increased malignancy of PC. Check for active clinical trials using this agent. (NCI Thesaurus)

A topical gel containing a peptide derived from the human papillomavirus (HPV). Application of 851B gel may stimulate the host immune system to trigger a cytotoxic T-lymphocyte response to cells that express HPV. Check for active clinical trials using this agent. (NCI Thesaurus)

A sulfate salt form of abacavir, a nucleoside reverse transcriptase inhibitor analog of guanosine. This agent decreases HIV viral loads, retards or prevents the damage to the immune system, and reduces the risk of developing AIDS. Check for active clinical trials using this agent. (NCI Thesaurus)

A murine IgG1 monoclonal anti-idiotype antibody, containing a variable antigen-binding region that functionally mimics the three-dimensional structure of a specific epitope on the ovarian cancer tumor-associated antigen CA-125, with potential antineoplastic activity. With a variable antigen-binding region that acts as a surrogate antigen for CA-125, abagovomab may stimulate the host immune system to elicit humoral and cellular immune responses against CA-125-positive tumor cells, resulting in inhibition of tumor cell proliferation.
Check for active clinical trials using this agent. (NCI Thesaurus)

A synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth. Check for active clinical trials using this agent. (NCI Thesaurus)

A novel, broad-spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. Abexinostat inhibits several isoforms of HDAC, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; and the tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis.
HDAC, upregulated in many tumor types, is an an enzyme that is responsible for the deacetylation of chromatin histone proteins. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally active acetate salt of the steroidal compound abiraterone with antiandrogen activity. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels.
Check for active clinical trials using this agent. (NCI Thesaurus)

An isotonic, sterile, absorbable adhesion barrier gel composed of polyethylene oxide and sodium carboxymethylcellulose, with protective activity. Upon application of a single layer into the uterine cavity at the end of any hysteroscopic surgery, the absorbable adhesion barrier gel may provide a protective barrier which protects the traumatized tissue and allows for healing. This gel may therefore prevent the formation of post-surgical intrauterine adhesions.
Check for active clinical trials using this agent. (NCI Thesaurus)

A sterile, absorbable surgical sealing patch composed of an equine collagen sponge coated with the coagulation factors human fibrinogen and human thrombin, with potential hemostatic activity. Applied on the wound tissue, the absorbable fibrin sealant patch adheres to the tissue and the solid fibrinogen and thrombin dissolve upon contact with the physiological fluid. In turn, fibrinogen is converted to fibrin monomers by thrombin, and polymerize to form a fibrin clot at the wound surface. This causes the patch to adhere to the wound surface and promotes tissue sealing. This may reduce lymphatic drainage and prevent seroma formation. Check for active clinical trials using this agent. (NCI Thesaurus)

A sterile hemostatic agent composed of purified porcine-derived gelatin. In regional chemotherapy, absorbable gelatin sponge may be used to embolize arteries in the region of a tumor in order to block or retard blood flow; this blockage results in a locally increased concentration of chemotherapeutic agents delivered to the tumor when chemotherapeutic agents are infused into the embolized arterial circulation upstream of the blockage. Check for active clinical trials using this agent. (NCI Thesaurus)

A hemostatic powder composed of hydrophilic, absorbable modified polymers (AMPs) derived from plant starch, with potential anti-hemorrhagic activity. Upon local administration of the AMP hemostatic powder directly sprayed over the bleeding surface, this powder adheres to the bleeding area, and the AMPs are able to absorb fluid and therefore soak up blood at the bleeding site. This leads to the formation of a gelled matrix that seals the affected site, and allows platelets, red blood cells and clotting factors in the blood to concentrate at the wound. In turn, this promotes the coagulation cascade, helps to stop or control bleeding, and prevents further blood loss. The AMP particles are naturally degraded by human enzymes over time. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally bioavailable antimitotic sulfonamide. ABT-751 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication. This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect. Check for active clinical trials using this agent. (NCI Thesaurus)

A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin), bleomycin, vinblastine and dacarbazine, used alone or in combination with radiation therapy, for the primary treatment of Hodgkin lymphoma. (NCI Thesaurus)

A regimen consisting of doxorubicin, bleomycin, vincristine, etoposide, prednisone and cyclophosphamide, given in combination with radiation therapy and used for the treatment of high-risk, childhood Hodgkin's lymphoma. (NCI Thesaurus)

A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin) and cyclophosphamide used in the adjuvant setting for the primary treatment of breast cancer. This regimen is also used for the treatment of recurrent and metastatic breast cancer. (NCI Thesaurus)

A 5-aminoimidazole-4-carboxamide (AICA) riboside, a purine nucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic activity. Following cellular uptake, acadesine is phosphorylated to AICA ribotide (ZMP), which mimics 5'-adenosine monophosphate (AMP). Both AMP-activated protein kinase (AMPK) and AMPK kinase (AMPKK) are activated by ZMP, which appears to be necessary for the induction of apoptosis. Acadesine-induced apoptosis also appears to require cytochrome c release from mitochondria and caspase activation and is p53-independent. However, the exact mechanism of acadesine-induced apoptosis is unknown. T cells are significantly less susceptible than B cells to acadesine-induced apoptosis. AMPK regulates several cellular systems including the cellular uptake of glucose, the beta-oxidation of fatty acids, protein synthesis, and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria. Check for active clinical trials using this agent. (NCI Thesaurus)

A juice product obtained from the fruit of the acai palm tree (Euterpe oleracea) with anti-inflammatory, antioxidant and potential chemopreventive activities. Besides high amounts of vitamins, minerals and fatty acids, acai berry is rich in phytonutrients such as anthocyanins and flavones which are potent scavengers of reactive oxygen species. The fruit also contains high amounts of the flavone velutin which exhibits potent anti-inflammatory properties. Velutin is able to inhibit the degradation of the inhibitor of nuclear factor kappa-B (NF-kB), thereby blocking the activation of NF-kB, as well as inhibiting phosphorylation of mitogen-activated protein kinase p38 and JNK. Inhibition of these processes results in suppression of the production of proinflammatory cytokines, such as tumor necrosis factor alpha and interleukin 6. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally available inhibitor of Bruton’s tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, acalabrutinib inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

A pseudotetrasaccharide and inhibitor of alpha-glucosidase and pancreatic alpha-amylase with antihyperglycemic activity. Acarbose binds to and inhibits alpha-glucosidase, an enteric enzyme found in the brush border of the small intestines that hydrolyzes oligosaccharides and disaccharides into glucose and other monosaccharides. This prevents the breakdown of larger carbohydrates into glucose and decreases the rise in postprandial blood glucose levels. In addition, acarbose inhibits pancreatic alpha-amylase which hydrolyzes complex starches to oligosaccharides in the small intestines. Check for active clinical trials using this agent. (NCI Thesaurus)

A human dermis-derived allograft material. Acellular cadaveric dermal matrix (ACDM) is derived from human cadaveric dermis from which the epidermis, all viable cells and major histocompatibility class (MHC) II antigens have been removed to minimize alloimmunogenicity, while the dermal collagen matrix is preserved. ACDM may placed over wounds to aid as a substitute for skin when necessary such as for surgical reconstruction or for protection against wound exposure and breakdown and wound infection. Check for active clinical trials using this agent. (NCI Thesaurus)

A 4-hydroxycoumarin derivative with anticoagulant activity. As a vitamin K antagonist, acenocoumarol inhibits vitamin K epoxide reductase, thereby inhibiting the reduction of vitamin K and the availability of vitamin KH2. This prevents gamma carboxylation of glutamic acid residues near the N-terminals of the vitamin K-dependent clotting factors, including factor II, VII, IX, and X and anticoagulant proteins C and S. This prevents their activity and thus thrombin formation. Compared to other coumarin derivatives, acenocoumarol has a short half-life. Check for active clinical trials using this agent. (NCI Thesaurus)

A p-aminophenol derivative with analgesic and antipyretic activities. Although the exact mechanism through which acetaminophen exert its effects has yet to be fully determined, acetaminophen may inhibit the nitric oxide (NO) pathway mediated by a variety of neurotransmitter receptors including N-methyl-D-aspartate (NMDA) and substance P, resulting in elevation of the pain threshold. The antipyretic activity may result from inhibition of prostaglandin synthesis and release in the central nervous system (CNS) and prostaglandin-mediated effects on the heat-regulating center in the anterior hypothalamus. Check for active clinical trials using this agent. (NCI Thesaurus)

The sodium salt of acetazolamide, a nonbacteriostatic sulfonamide derivative with diuretic and anticonvulsant properties. Acetazolamide is a potent inhibitor of carbonic anhydrase that plays an important role in the control of fluid secretion. Inhibition of this enzyme in the kidney results in a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen, thereby leading to increased bicarbonate and cation excretion, and increased urinary volume. Reduced bicarbonate level in circulation induces reduction of intraocular pressure via osmotic mechanism. The anticonvulsant activity of acetazolamide may contribute to inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. Check for active clinical trials using this agent. (NCI Thesaurus)

A synthetic carboxylic acid with antibacterial and antifungal properties. Although its mechanism of action is not fully known, undissociated acetic acid may enhance lipid solubility allowing increased fatty acid accumulation on the cell membrane or in other cell wall structures. Acetic acid, as a weak acid, can inhibit carbohydrate metabolism resulting in subsequent death of the organism. Check for active clinical trials using this agent. (NCI Thesaurus)

An intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide. Check for active clinical trials using this agent. (NCI Thesaurus)

A synthetic N-acetyl derivative of the endogenous amino acid L-cysteine, a precursor of the antioxidant enzyme glutathione. Acetylcysteine regenerates liver stores of glutathione. This agent also reduces disulfide bonds in mucoproteins, resulting in liquification of mucus. Some evidence suggests that acetylcysteine may exert an anti-apoptotic effect due to its antioxidant activity, possibly preventing cancer cell development or growth. In addition, acetylcysteine has inhibited viral stimulation by reactive oxygen intermediates, thereby producing antiviral activity in HIV patients. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally bioavailable combination pill containing aspirin, simvastatin, atenolol, ramipril and thiazide with preventive activity against cardiovascular disease (CVD). Aspirin is a cyclooxygenase inhibitor with antiplatelet, analgesic, antipyretic and anti-inflammatory activities; simvastatin is a statin with a cholesterol lowering effect; and the beta-blocker atenolol as well as the ACE inhibitor ramipril and the thiazide diuretic all have blood pressure lowering activity. Upon oral administration of aspirin/simvastatin/atenolol/ramipril/thiazide capsule, the combined effects of the active ingredients in this formulation lower the risk of CVD. Check for active clinical trials using this agent. (NCI Thesaurus)

An oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus. Aclarubicin intercalates into DNA and interacts with topoisomerases I and II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin. Check for active clinical trials using this agent. (NCI Thesaurus)

A synthetic imidazoquinoline with antineoplastic activity. Acodazole intercalates into DNA, resulting in disruption of DNA replication. Use of this agent has been associated with significant cardiotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)

A brain mimicking fluid with an attenuation coefficient similar to that found in the adult human brain, which can potentially improve the quality of an image acquired during intraoperative ultrasonography. Upon administration into the resection cavity during surgical removal of a brain tumor, the acoustic coupling fluid may both increase the quality of the ultrasound image and improve the visualization of the tumor. This may facilitate the surgical removal of residual tumor while sparing normal, healthy brain tissue.
Check for active clinical trials using this agent. (NCI Thesaurus)

A tricyclic acridine-based (or carboxamide-based) drug with dual topoisomerase inhibitor and potential antineoplastic activities. Acridine carboxamide inhibits both topoisomerases I and II and intercalates into DNA, resulting in DNA damage, the disruption of DNA repair and replication, the inhibition of RNA and protein synthesis, and cell death. Check for active clinical trials using this agent. (NCI Thesaurus)

A chemotherapy regimen consisting of doxorubucin hydrochloride (Adriamycin) and cyclophosphamide, followed by paclitaxel (Taxol), administered on either a dose-dense or sequential schedule and used as an adjuvant treatment for breast cancer. (NCI Thesaurus)

A preparation of cells, which consists of autologous marrow infiltrating lymphocytes (MILs), that are manipulated in vitro, with potential antitumor and immune stimulating activities. MILs are harvested from autologous bone marrow from multiple myeloma patients and, in vitro, are exposed to and activated by anti-CD3/anti-CD28 monoclonal antibodies covalently attached to super-paramagnetic microbeads. After removal of the beads and expansion of the cells in culture, the activated MILs (aMILs) are re-introduced into the patient. The aMILs possess enhanced myeloma specificity, and are able to infiltrate the tumor microenvironment and initiate tumor cell lysis. CD3 and CD28, co-stimulatory molecules expressed on the surface of T-lymphocytes, play a key role in the activation of T-cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A soluble fusion protein containing the extracellular domain of the activin receptor type 2B (ACVR2B or ActRIIB) fused to a human Fc domain, with potential antineoplastic activity. Upon intravenous administration, STM 434 selectively binds to the growth factor activin A, thereby preventing its binding to and the activation of endogenous ActRIIB. This prevents activin A/ActRIIB-mediated signaling and inhibits the proliferation of activin A-overexpressing tumor cells. Activin A, a member of the transforming growth factor beta (TGF-beta) superfamily, is overexpressed in a variety of cancers and plays a key role in promoting cancer cell proliferation, migration, and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

The sodium salt form of acyclovir, a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses. After conversion in vivo to the active metabolite acyclovir triphosphate, acyclovir competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the thymidine kinase of HSV. Check for active clinical trials using this agent. (NCI Thesaurus)

The sodium salt form of acyclovir, a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses of the herpesvirus family. After conversion in vivo to the active metabolite acyclovir triphosphate by viral thymidine kinase, acyclovir competitively inhibits viral DNA polymerase by incorporating into the growing viral DNA chain and terminating further polymerization. Check for active clinical trials using this agent. (NCI Thesaurus)

A recombinant type 5 adenovirus (Ad5), encoding the gene for the human sodium-iodide symporter (NIS) linked to the cytomegalovirus (CMV) promoter, with potential gene transfection activity. Upon intratumoral injection, Ad5-CMV-NIS is taken up by tumor cells, resulting in the cellular expression of NIS. Subsequently, orally administered iodine 131 is taken up by NIS-expressing tumor cells, which may result in the selective accumulation of a cytotoxic dose of beta and gamma radiation in non-thyroidal tumor cells, sparing adjacent normal tissue. NIS, an intrinsic membrane glycoprotein, is an ion pump that actively transports iodide into cells which concentrate iodine; in addition to thyroid epithelial cells, it is found in non-thyroidal tissues including the salivary glands, the gastric mucosa, and lactating mammary glands. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-defective adenoviral-CMV vector that encodes a wild-type p53 gene. Ad5CMV-p53 induces tumor cells that have been transfected with the vector to produce wild-type p53, a tumor suppressor gene that is deleted or mutated in a significant number of cancers. In transfected tumor cells, the wild-type p-53 gene product exerts an antitumor effect by blocking cell cycle progression at the G1/S regulation point, activating DNA repair proteins in the presence of DNA damage, and initiating apoptosis when DNA damage is irreparable. Check for active clinical trials using this agent. (NCI Thesaurus)

A cell-based cancer vaccine containing autologous dendritic cells (DCs) that are transduced with a replication-deficient adenovirus type 5 vector (Ad5) encoding a mutated form of the tumor-associated antigen (TAA) survivin, with potential immunostimulatory and antineoplastic activities. Upon administration, Ad5-survivin-transduced autologous DC vaccine may elicit an immune response against cancer cells expressing survivin by activating cytotoxic T cells (CTLs). This leads to an induction of cell death in survivin-positive tumor cells. Survivin, a member of the inhibitor of apoptosis (IAP) family of proteins, may be upregulated in certain tumor cell types and plays a key role in tumor cell growth and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally bioavailable adenosine A2A receptor (A2AR) antagonist, with potential antineoplastic activity. Upon administration, A2AR antagonist PBF-509 selectively binds to and inhibits A2AR expressed on T lymphocytes. This abrogates the adenosine/A2AR-mediated inhibition of T-lymphocytes and activates a T-cell-mediated immune response against tumor cells, thereby reducing proliferation of susceptible tumor cells. A2AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of T-cells and, upon activation by adenosine, inhibits their proliferation and activation. Adenosine is often produced in excess by cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A genetically-modified, dendritic cell (DC)-based vaccine in which the autologous cells are transduced with an adenoviral vector expressing the tumor antigen prostate-specific membrane antigen (PSMA) and a fusion protein composed of synthetic ligand inducible adjuvant iMC composed of a drug-inducible costimulatory CD40 receptor (iCD40) and the adaptor protein MyD88, with potential immunomodulating and antineoplastic activities. The iCD40 contains a membrane-localized cytoplasmic CD40 domain fused to the FK506 modified drug-binding protein 12 (FKBP12). Upon intradermal administration of BPX-201, these DCs accumulate in local draining lymph nodes. Twenty-four hours after vaccination, the dimerizing agent AP1903 is administered. AP1903 binds to the drug binding domain, leading to iMC oligomerization and activation of iCD40 and MyD88-mediated signaling in iMC-expressing DCs. This signaling pathway activates the DCs and stimulates a cytotoxic T-lymphocyte (CTL) response against host tumor cells that express PSMA. PSMA, a glycoprotein secreted by prostatic epithelial and ductal cells, is overexpressed in prostate cancer cells and is used as a tumor marker for both diagnosis and treatment evaluation. MyD88 is involved in interleukin 1 receptor (IL1R) and toll-like receptor (TLR) signaling. Check for active clinical trials using this agent. (NCI Thesaurus)

A therapeutic cancer vaccine composed of a replication-defective, serotype 5 adenovirus (Ad5) with the viral genes early 1 (E1), early 2b (E2b), and early 3 (E3) deleted, and the human transcription factor brachyury encoded, with potential immunostimulating and antineoplastic activities. Upon subcutaneous administration, the adenoviral brachyury vaccine ETBX-051 expresses the brachyury protein. The expressed brachyury may induce a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells expressing brachyury, thereby resulting in both immune-mediated inhibition of tumor cell proliferation and tumor cell death. Deletion of the E1, E2b and E3 genes from Ad5 prevents anti-adenovirus immune responses. Brachyury, a tumor-associated antigen (TAA) and member of the T-box family of transcription factors, is overexpressed in a variety of tumor types. It plays an important role in cancer progression and metastasis.

A therapeutic cancer vaccine composed of a replication-defective, serotype 5 adenovirus (Ad5) with the viral genes early 1 (E1), early 2b (E2b), and early 3 (E3) deleted, and the human glycoprotein mucin 1 (MUC1) encoded, with potential immunostimulating and antineoplastic activities. Upon subcutaneous administration, the adenoviral MUC1 vaccine ETBX-061 expresses the MUC1 protein. The expressed MUC1 may induce a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells expressing MUC1, thereby resulting in both immune-mediated inhibition of tumor cell proliferation and tumor cell death. Deletion of the E1, E2b and E3 genes from Ad5 prevents anti-adenovirus immune responses. MUC1, a tumor-associated antigen (TAA) and type I transmembrane protein, is overexpressed in a variety of tumor types. It plays an important role in cancer progression and metastasis.

Autologous dendritic cells tranduced with a replication incompetent adenovirus encoding human pro-inflammatory cytokine interleukin-12 (IL-12) (INXN-3001) in combination with the proprietary orally bioavailable, small molecule activator ligand INXN-1001, with potential immunomodulating and antineoplastic activities. Production of IL-12 is controlled by an inducible DNA element that allows transcription initiation only in the presence of the ligand inducer INXN-1001. Upon intratumoral injection of INXN-3001 and subsequent oral administration of activator ligand, INXN-1001 is able to induce expression of IL-12 in INXN-3001. IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells, inducing the secretion of interferon-gamma and inducing a cytotoxic T lymphocyte response against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. As INXN-1001 regulates both the timing and the levels of IL-12 expression, IL-12 toxicity can be reduced. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-defective, recombinant adenoviral serotype 5 (Ad5) encoding human guanylyl cyclase C (hGCC) and the synthetic Pan DR epitope (PADRE), with potential antineoplastic and immunomodulating activities. Upon intramuscular administration, the Ad5-hGCC-PADRE vaccine expresses hGCC, which may induce both humoral and cellular immune responses against tumor cells expressing the hGCC antigen. This results in the immune-mediated inhibition of tumor cell proliferation, and leads to tumor death. The hGCC protein is normally restricted to intestinal epithelial cells but is overexpressed by metastatic colorectal tumors. PADRE is a helper T-lymphocyte epitope that is able to augment the magnitude and duration of the cytotoxic T-lymphocyte (CTL) response. Check for active clinical trials using this agent. (NCI Thesaurus)

A gene-viral vector complex comprised of an adenovirus vector and B7-1 gene targeting the CD80 antigen. Adenovirus B7-1 is used as a component in antineoplastic vaccines to elicit a cytotoxic T-cell response. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-deficient, recombinant adenovirus encoding human aquaporin-1 with potential membrane water channel activity. Upon transfection of salivary glands, adenovirus encoding human aquaporin-1 (AdhAQP1) directs human aquaporin-1 (hAQP1) expression in the apical and basolateral plasma membranes of salivary secretory cells, which may result in increased saliva production. hAQP1, a water channel protein, is one of several highly conserved water channel proteins that mediate water permeability in cells of water-transporting tissues. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-defective oncolytic adenovirus, encoding rat Her-2/neu (ErbB-2), with potential antineoplastic activity. Upon administration, adenovirus encoding rat HER-2/neu may induce an immune response against tumor cells expressing the HER-2/neu antigen, which may result in the immune-mediated inhibition of tumor cell proliferation and tumor cell death. Her-2/neu, a tumor-associated antigen and member of the epidermal growth factor receptor (EGFR) family of tyrosine kinases, is overexpressed in various tumor cell types. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-defective, recombinant oncolytic adenovirus encoding human endostatin with potential antineoplastic activity. Endostatin, a 20 kDa C-terminal proteolytic fragment of collagen XVIII, is an important angiogenesis inhibitor. Upon intratumoral administration, the adenovirus infects and replicates in tumor cells. The expressed endostatin may inhibit endothelial cell proliferation and angiogenesis which may result in a reduction of tumor growth. Check for active clinical trials using this agent. (NCI Thesaurus)

One of a number of genetically-engineered adenoviruses designed to insert a gene of interest into a eukaryotic cell where the gene of interest is subsequently expressed. Unlike most other vectors, adenovirus vectors have the ability to infect post-mitotic cells. Thus, these agents are especially useful for gene transfer into neuronal cells. Check for active clinical trials using this agent. (NCI Thesaurus)

Allogeneic tri-viral specific, adenovirus, cytomegalovirus and Epstein-Barr virus (Adv, CMV and EBV or ACE), cytotoxic T-lymphocytes (CTLs) with potential antiviral activity. Donor-derived T-cells were exposed to dendritic cells nucelofected with DNA plasmids encoding Hexon and Penton (Adv), pp65 and IE1 (CMV), and LMP2, EBNA1 and BZLF1 (EBV), all are critical proteins for the proliferation of these viruses, and subsequently maintained in the presence of interleukins 4 and 7 with a novel culture device to expand and sustain the repertoire of CTLs. After an allogeneic hematopoietic stem cell transplant (HSCT), infusion of these CTLs primed towards Adv, CMV and EBV may prevent viral infection by these pathogens.

A nanoparticle-based formulation containing a recombinant non-replicating adenovirus (Ad) encoding toll-like receptor 5 (TLR5) and its specific ligand protein 502S, with potential antineoplastic and immunomodulating activities. Upon administration, the Ad preferentially and specifically infects cells expressing the Coxsackievirus and adenovirus receptor (CAR), which is highly expressed in certain human tumors, and expresses both TLR5 and a specific agonistic ligand in the same cell. 502S binds to and activates TLR5, thereby allowing for continuous TLR5 signaling. This stimulates dendritic cells (DCs), monocytes, macrophages and the nuclear factor-kappa B (NF-κB) signaling cascade. This activation results in the production of pro-inflammatory cytokines, including interferon alpha, tumor necrosis factor-alpha and the interleukins (IL), IL-1 beta, -6 and -12. This may induce a T helper cell-1 (Th1) immune response and activate a cytotoxic T-lymphocyte (CTL) response against tumor associated antigens (TAAs). TLR5, a member of the TLR family, plays a key role in the activation of innate immunity.
Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-incompetent adenovirus encoding human pro-inflammatory cytokine interleukin-12 (IL-12) (Ad.hIL-12), with potential immunomodulating and antineoplastic activities. Upon intratumoral administration, the adenovirus selectively infects and replicates in tumor cells, which may result in tumor cell lysis. Synergistically, IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells (NKs), inducing secretion of interferon-gamma and inducing cytotoxic T cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication incompetent adenovirus encoding the human pro-inflammatory cytokine interleukin-12 (IL-12) (INXN-2001) in combination with the proprietary activator ligand veledimex, with potential immunomodulating and antineoplastic activities. Production of IL-12 is controlled by an inducible DNA element that allows transcription initiation only in the presence of the ligand inducer. Upon intratumoral administration of INXN-2001 and oral administration of veledimex, veledimex is able to induce expression of IL-12 from INXN-2001. IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells (NKs), inducing secretion of interferon-gamma and inducing cytotoxic T cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation.

A cancer vaccine composed of a genetically engineered, replication-deficient type 5 adenovirus carrying the human prostate-specific antigen (PSA), with potential immunostimulating and antineoplastic activities. Upon subcutaneous vaccination with the adenovirus-PSA prostate cancer vaccine, the adenovirus infects cells and expresses PSA. In turn, PSA may activate the immune system and may induce a cytotoxic T-lymphocyte response against PSA-expressing tumor cells. PSA, a tumor associated antigen, is expressed by prostate epithelial cells and is overexpressed in prostate cancer. Check for active clinical trials using this agent. (NCI Thesaurus)

Autologous dendritic cells (DCs) transduced with a recombinant, replication-defective adenoviral vector expressing the fusion gene granulocyte-macrophage colony-stimulating factor (GM-CSF) and carbonic anhydrase IX (CA-IX or CA9) (GMCA-9), with potential immunomodulating activity. The autologous DCs are transduced ex vivo and express the GMCA-9 fusion protein on the cell surface. Upon intradermal administration of the AdGMCAIX-transduced autologous DCs back into the patient, the DCs activate the immune system to both mount a cytotoxic T lymphocyte-mediated response against tumor cells positive for the CA9 antigen, and generate memory T cells. This may result in decreased tumor growth. CA9, also known as G250, is a renal cell carcinoma (RCC)-associated antigen and a member of the carbonic anhydrase family that contains a human leukocyte antigen (HLA)-A2.1-restricted epitope; it is found in a majority of renal cell carcinomas while absent in most normal tissues. The cytokine GM-CSF enhances the immunogenicity of CA9-based DC vaccines. Check for active clinical trials using this agent. (NCI Thesaurus)

A small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell-cell adhesion and signaling mechanisms; may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels. Check for active clinical trials using this agent. (NCI Thesaurus)

A human serotype 5, replication-defective, first generation adenoviral vector, with the viral E1a and E3 protein encoding regions deleted, which is engineered to express the soluble, immune-mediated stimulatory gene human fms-like tyrosine kinase 3 ligand (Flt3L), under the transcriptional control of the CMV promoter, with potential immunostimulating activity. Upon administration, Ad-hCMV-Flt3L is transduced into tumor cells and Flt3L is expressed. Flt3L stimulates both the proliferation of dendritic cells (DCs) and their migration to the tumor site. Upon exposure to the tumor-associated antigens (TAA) released from dying glioma cells, which were killed by thymidine kinase-mediated valacyclovir-induced tumor cell death, the DCs initiate a specific immune response against any remaining TAA-expressing tumor cells. Flt3L is a hematopoietic growth factor and ligand for the Flt3 tyrosine kinase receptor. Check for active clinical trials using this agent. (NCI Thesaurus)

A population of cells derived from adipose tissue with stem cell and wound repair activities. Adipose-derived regenerative cells (ADRC) consists of several cell types, such as adult stem cells, vascular endothelial cells, and vascular smooth muscle cells, among others. These cells contribute to wound repair through a variety of mechanisms by promoting blood vessel growth and blocking apoptosis. In addition, ADRC can differentiate into several tissue types, such as bone, cartilage, fat, skeletal muscle, smooth muscle and cardiac muscle. Check for active clinical trials using this agent. (NCI Thesaurus)

A population of stromal vascular fraction (SVF) cells derived from autologous adipose tissue, with potential tissue regenerative activity. SVF cells are obtained through liposuction and contain multiple cell types, including adipose-derived stem cells (ADSCs), mesenchymal and endothelial progenitor cells, leukocyte subtypes, lymphatic cells, pericytes, and vascular smooth muscle cells. The SVF cells are processed in such a way as to contain a reproducible and consistent composition of heterogeneous cells. Upon processing and administration, the adipose-derived SVF cells can differentiate into different tissue types, support neovascularization, replace cells and repair injured issue. Check for active clinical trials using this agent. (NCI Thesaurus)

A replication-defective adenovirus vector (Ad-ISF35), which encodes a membrane-stabilized, chimeric human-mouse CD40 binding protein (CD40 ligand; CD40L; CD154), with potential immunomodulatory and antineoplastic activities. Upon intratumoral administration, Ad-ISF135 preferentially transduces tumor cells and immunoregulatory cells in the tumor microenvironment. This increases the expression of CD154 in tumor cells, activates CD40 and stimulates signaling and immunoactivation, which are both mediated by CD40. This increases the expression of co-stimulatory molecules on these cells, which enhances their ability to function as antigen presenting cells (APCs) and increases their apoptotic potential. This leads to an increase in the infiltration of macrophages and neutrophils, which promote direct cytotoxicity, enhances the production of pro-inflammatory cytokines in the tumor microenvironment, and induces a specific cytotoxic T-lymphocyte (CTL) response against the tumor cells. In addition, transduction with Ad-ISF35 induces direct tumor cell death, probably through an anti-viral immune response. Ad-ISF35 also exerts a strong bystander effect in non-transduced cells thereby further inducing tumor cell death. Altogether, this will eradicate tumor cells. CD154, the main ligand for CD40, plays a key role in the activation of APCs, promotes immunoactivation, and increases apoptotic potential. The protein encoded by Ad-ISF35 does not contain the mouse antibody binding domains and does not induce human neutralizing antibodies. The metalloprotease cleavage site is deleted in this chimeric CD154 and thus it resists cleavage; the encoded protein also contains amino acid substitutions within the carboxy-terminal. Both sets of engineered mutations promote cell surface expression. Check for active clinical trials using this agent. (NCI Thesaurus)

An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surface surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers. Check for active clinical trials using this agent. (NCI Thesaurus)

An alkylating agent that bind to the DNA minor groove in a sequence-specific manner and form covalent adducts with adenines, resulting in the inhibition of DNA replication and induction of apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)

A hormone secreted by the anterior portion of the pituitary gland and regulates hormone, primarily cortisol, secreted by the adrenal gland. Check for active clinical trials using this agent. (NCI Thesaurus)

An inducible adenoviral vector encoding human pro-inflammatory cytokine interleukin-12 (IL-12; IL12), which is under the transcriptional control of the RheoSwitch Therapeutic System (RTS) (Ad-RTS-hIL-12), with potential immunomodulating and antineoplastic activities. RTS consists of two fusion proteins: Gal4-EcR, which contains a modified ecdysone receptor (EcR) fused with the DNA binding domain of the yeast Gal4 transcription factor, and VP16-RXR, which contains a chimeric retinoid X receptor (RXR) fused with the transcription activation domain of the viral protein VP16 of herpes simplex virus type 1 (HSV1). Upon intratumoral administration of Ad-RTS-hIL-12, given in combination with the proprietary, diacylhydrazine-based activator ligand veledimex (INXN-1001), veledimex binds specifically to the EcR part of the RTS and stabilizes heterodimerization between the two fusion proteins, forming an active transcription factor, which induces the transcription of IL-12 under the control of an inducible promoter containing Gal4-binding sites. The expressed IL-12 activates the immune system by promoting the activation of natural killer cells (NK cells), inducing secretion of interferon-gamma (IFN-g) and inducing cytotoxic T-lymphocyte (CTL)-mediated responses against tumor cells, which may result in immune-mediated tumor cell lysis and inhibition of tumor cell proliferation. In the presence of veledimex, the protein heterodimer changes to a stable conformation and can bind to the inducible promoter, while without veledimex the two fusion proteins form unstable heterodimers; this allows the controlled, regulated intratumoral expression of the IL-12 gene.

A cell-based vaccine comprised of prostate cancer cells transduced with an adenoviral vector encoding human RTVP-1 (AdRTVP-1), with potential immunostimulating and antineoplastic activities. RTVP-1, also referred to as glioma pathogenesis-related protein 1 (GLIP1), is down-regulated in prostate tumors. Regulated by tumor suppressor p53, the expression of RTVP-1 functions as a tumor suppressor, and is abundant in normal human prostate epithelial cells as well as in differentiated macrophages. Administration of AdRTVP-1-transduced prostate cancer cell-based vaccine leads to an induction of apoptosis through the expression of RTVP-1, which may result in a reduction in prostate cancer cellular proliferation. In addition, this vaccine may induce a cytotoxic T lymphocyte (CTL) response against prostate specific tumor- associated antigens. Check for active clinical trials using this agent. (NCI Thesaurus)

A cancer vaccine consisting of a recombinant adenoviral vector encoding the tumor-associated antigen (TAA) human MUC-1 (hMUC-1) linked to the extracellular domain (ecd) of the co-stimulatory molecule CD40 ligand (CD40L) and an adenovirus signal sequence that encodes a secretory signal peptide (Ad-sig) with potential immunostimulating and antineoplastic activities. Due to the presence of the secretory signal peptide expressed by Ad-sig in the vaccine construct, transfected cells may secrete a fusion protein composed of hMUC-1 and the CD40L ecd. The CD40L moiety part of the fusion protein binds to CD40 receptors on dendritic cells (DCs). Subsequently, DCs may be activated and migrate, T-cells may expand, and a cytotoxic T lymphocyte (CTL) response against tumor cells that overexpress hMUC-1 may follow. MUC-1 is a hypoglycosylated TAA overexpressed by epithelial cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A second-generation synthetic antisense oligonucleotide with potential antineoplastic activity. AEG35156 selectively blocks the cellular expression of X-linked inhibitor of apoptosis protein (XIAP), a pivotal inhibitor of apoptosis that is overexpressed in many tumors. This agent reduces total levels of XIAP in tumor cells, working synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. XIAP interferes with both the intrinsic and extrinsic program-death signaling pathways, which may render tumor cells resistant to apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)

An aerosol formulation of aldesleukin, a recombinant form of interleukin-2 (IL-2), with potential immunostimulating activity. Upon IL-2 inhalation, this cytokine activates lymphokine-activated killer cells and natural killer cells, and induces expression of cytotoxic cytokines, such as interferon-gamma and transforming growth factor-beta. This may eventually halt tumor cell growth. Localized administration of IL-2 may decrease toxicity and increase efficacy. Check for active clinical trials using this agent. (NCI Thesaurus)

The dimaleate salt form of afatinib, an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Check for active clinical trials using this agent. (NCI Thesaurus)

A tamoxifen metabolite with both estrogenic and anti-estrogenic effects. Afimoxifene has a higher affinity for the estrogen receptor than tamoxifen, and functions as an antagonist in breast cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A cancer vaccine composed of naked plasmid DNA of the gene for the tumor-associated antigen alpha-fetoprotein (AFP), a macromolecule that acts as a specific immunologic target for hepatocellular carcinoma. This agent exerts an antitumor effect by inducing cytotoxic T-lymphocytes to attack AFP-expressing tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

A synthetic lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and antineoplastic activities. AFP464 is rapidly converted to aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in cytochrome P450 1A1 (CYP1A1) and cytochrome P450 1A2 (CYP1A2) expression and, to a lesser extent, an increase in cytochrome P450 1B1 (CYP1B1) expression. Subsequently, aminoflavone is metabolized to toxic metabolites by the cytochromome P450 enzymes that it induces; these toxic metabolites covalently bind to DNA, resulting in the phosphorylation of p53, the induction of the p53 downstream target p21Waf1/Cip1, and apoptosis. Pulmonary toxicity may be dose-limiting. Check for active clinical trials using this agent. (NCI Thesaurus)

An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Afuresertib binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. Check for active clinical trials using this agent. (NCI Thesaurus)